Featured Products 2009

Highlighted products added to the Tocris Bioscience range during 2009

December 2009

Selective ERβ agonist
3366 | WAY 200070

Displays 68-fold selectivity over ERα (EC50 values are 2 and 155 nM for ERβ and ERα respectively). Displays antianxiolytic and antidepressive effects in vivo.

Related Products: PHTPP DPN PPT
Selective Rho-kinase (ROCK) inhibitor
3726 | GSK 429286

IC50 values are 14, 780 and 1940 nM for ROCK1, RSK and p70S6K respectively. Reverses adrenalin-induced contraction of the rat aortic ring (IC50 = 190 nM) and causes a dose-dependent decrease in mean arterial blood pressure in spontaneous hypertensive rats. Orally active.

Related Products: Y-27632 Glycyl-H 1152
Selective positive allosteric modulator at mGlu4
3707 | VU 0361737

EC50 values are 240 and 110 nM at human and rat receptors respectively. Inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. Brain penetrant.

Related Products: SIB 1893 MPEP VU 0155041 sodium salt
Potent and highly selective GPR30 agonist
3577 | G-1

Ki = 11 nM, EC50 = 2 nM. Displays no activity at ERα and ERβ at concentration up to 10 μM. Inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants (IC50 values are 0.7 and 1.6 nM respectively) in vitro.

Related Products: Tamoxifen citrate ICI 182,780 β-Estradiol
Potent DNA-dependent protein kinase inhibitor
3712 | NU 7441

IC50 values are 14, 1700, 5000, >100000 and >100000 nM for DNA-PK, mTOR, PI 3-K, ATM and ATR respectively. Potentiates the effects of radiation, doxorubicin and etoposide in human tumor cell lines in vitro and etoposide in a human tumor xenograft model in vivo.

Related Products: NU 7026 DMNB Compound 401

November 2009

Potent and selective CB1 antagonist
3676 | PF 514273

Ki values are 1 and > 10000 nM at CB1 and CB2 receptors respectively. Inhibits food intake in vivo following oral administration.

Related Products: AM 251 LY 320135 O-2050
Selective FGFR1 and -3 inhibitor
3044 | PD 173074

IC50 values are 5, 21.5, ~100, 17600 and 19800 nM for FGFR3, FGFR1, VEGFR2, PDGFR and c-Src respectively. Inhibits VEGF- and FGF-induced angiogenesis in the mouse cornea model of angiogenesis.

Related Products: SU 5402 SU 6668
Selective D2-like agonist
3680 | Ropinirole

D3 > D2 > D4. Causes biphasic spontaneous locomotor activity and contralateral circling in 6-OHDA-lesioned mice. Displays antiParkinsonian activity.

Related Products: (-)-Quinpirole Bromocriptine (S)-(-)-Sulpiride
Benzodiazepine site agonist
3655 | Zaleplon

Non-benzodiazepine agent that acts as an agonist at the benzodiazepine site. Displays hypnotic, anxiolytic, myorelaxant and anticonvulsant activity.

Related Products: L-655,708 Zolpidem Zopiclone
Dual site Src kinase inhibitor
3642 | Src I1

IC50 values are 44 and 88 nM for Src and Lck respectively. Can be used in parallel with PP 1 and PP 2 to inhibit Src family kinases.

Related Products: Piceatannol PP 2 PP 1

October 2009

Potent, competitive NPY Y1 antagonist
3242 | BMS 193885

Ki = 3.3 nM, IC50 = 5.9 nM. Displays > 47, > 100, > 160, > 160 and > 160-fold selectivity over σ1, α1, Y2, Y4 and Y5 receptors respectively. Reduces food intake and body weight via central Y1 inhibition and is brain penetrant.

Related Products: BIBO 3304 BIBP 3226 [Leu31,Pro34]-Neuropeptide Y (human, rat)
Peptide cleaved from PAR1 upon receptor activation
3554 | Parstatin (mouse)

Cell-permeable peptide cleaved from protease-activated receptor 1 (PAR1) upon receptor activation. Attenuates endothelial cell migration and proliferation (IC50 ~ 20 μM), and induces cell cycle arrest.

Related Products: TFLLR-NH2 TRAP-6 SCH 79797
Selective σ1 antagonist
3133 | NE 100

Ki = 0.86 nM. Displays > 55-fold selectivity over σ2 receptors and > 6000-fold selectivity over D1, D2, 5-HT1A, 5-HT2 and PCP receptors. Exhibits reversible binding (Kd = 1.2 nM) and displays antipsychotic activity in vivo. Orally active.

Related Products: BD 1047 (+)-SK&F 10047 PRE-084
Reverse transcriptase inhibitor
3666 | Tenofovir

Selectively inhibits HIV reverse transcriptase (RNA-dependent DNA polymerase). Prevents cytotoxicity in SIV-infected C-8166 cells in vitro (IC50 = 1.5 μM). Antiviral agent.

Related Products: Acyclovir DAPTA
Potent and selective NPY Y5 antagonist
3432 | S 25585

IC50 values are 5.4, > 1000, > 10 000 and > 10 000 nM at Y5, Y1, Y2 and Y4 receptors respectively. Significantly inhibits NPY-induced feeding but not through blockade of Y5 receptors.

Related Products: L-152,804 [cPP1-7,NPY19-23,Ala31,Aib32,Gln34] - hPancreatic Polypeptide CGP 71683

September 2009

Potent, orally active DPP-IV inhibitor
3506 | NVP DPP 728

Ki = 11 nM, IC50 = 14 nM. Displays > 15 000-fold selectivity over DPP-II and a range of proline-cleaving proteases. Exhibits antidiabetic activity in vivo.

Related Products: DPPI 1c K 579
Diacyl glycerolacyltransferase 1 (DGAT-1) inhibitor
3587 | A 922500

IC50 values are 7 and 24 nM at human and mouse DGAT-1 respectively. Devoid of activity at DGAT-2, ACAT1 or ACAT2. Induces significant weight loss without altering food intake, and decreases liver and plasma triglyceride levels in vivo. Orally active.

Potent Raf kinase inhibitor
3185 | L-779,450

IC50 = 10 nM. Displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively. Suppresses DNA synthesis and induces apoptosis in cells that proliferate in response to Raf-1 and A-Raf but not B-Raf.

Related Products: GW 5074 ZM 336372
Selective FAAH inhibitor
3307 | PF 750

IC50 = 16.2 nM. Displays no activity at a range of other serine hydrolases. Selectively inhibits FAAH within the central nervous system. Orally active.

Related Products: JNJ 1661010 AACOCF3
Potent and selective CB2 agonist
3088 | HU 308

Ki values are 22.7 nM and > 10 μM for CB2 and CB1 receptors respectively, EC50 = 5.57 nM. Displays antiallodynic activity in the rat hindpaw incision model of postoperative pain.

Related Products: JTE 907 GP 1a AM 630

August 2009

Potent and highly selective EP3 antagonist
3342 | L-798,106

Ki values are 0.3, 916, > 5000 and > 5000 nM at EP3, EP4, EP1 and EP2 respectively. Attenuates sulprostone-induced inhibition of EFS-evoked twitch and contractile responses in vivo.

Related Products: L-161,982 U 46619 Misoprostol
Orally active, selective 5-HT6 antagonist
3368 | SB 271046

pKi - 9.02 - 8.92. Increases extracellular glutamate and aspartate in the frontal cortex, and exhibits anticonvulsant activity (EC50 = 0.16 μM).

Related Products: EMD 386088 SB 399885 SB 258585
SGK inhibitor
3572 | GSK 650394

IC50 values are 62 and 103 nM for SGK1 and SGK2 respectively. Displays > 30-fold selectivity over Akt and other related kinases. Inhibits androgen-stimulated growth of LNCaP cells, a human prostate carcinoma cell line (IC50 ~ 1 μM).

Related Products: Bicalutamide Fluticasone Mifepristone
Potent AMPK activator
3336 | A 769662

EC50 = 0.8 μM. Displays selectivity towards β1 subunit-containing heterotrimers. Inhibits fatty acid synthesis (IC50 = 3.2 μM) and decreases plasma glucose and triglyceride levels in vivo.

Related Products: Dorsomorphin AICAR
GABAA receptor positive allosteric modulator
3597 | Indiplon

Ki = 1.2 - 1.7 nM. Acts at the benzodiazepine site. Displays ~ 10-fold selectivity for α1 subunit-containing receptors. Exhibits sedative, hypnotic, anxiolytic and anticonvulsant activity in vivo and is orally active.

Related Products: (-)-Bicuculline methochloride L-655,708 SR 95531

July 2009

Functionally selective M1 agonist
3569 | Xanomeline

EC50 values are 0.3, 5, 42, 52 and 92.5 nM at M1, M3, M5, M4 and M2 receptors respectively. Exhibits antipsychotic activity, and improves cognitive deficits and behavioural disturbances in Alzheimer's disease and schizophrenia.

Related Products: Pirenzepine Oxotremorine
Potent and selective amylin receptor antagonist
3419 | AC 187

IC50 = 0.48 nM. Displays 38-fold and 400-fold selectivity over calcitonin and CGRP receptors respectively. Increases glucagon secretion, accelerates gastric emptying, alters plasma glucose levels and increases food intake in vivo.

Related Products: CGRP 8-37 (rat) CGRP (rat) α-CGRP (human)
Potent and selective GlyT1 inhibitor
3397 | LY 2365109

IC50 values are 15.8 and > 30 000 nM at GlyT1 and GlyT2 respectively. Induces a dose-dependent elevation in CSF levels of glycine, and enhances acetylcholine and dopamine release in the striatum and prefrontal cortex respectively. Produces profound locomotor and respiratory impairments at higher doses.

Related Products: ALX 5407 NFPS Sarcosine
Potent FGFR and VEGFR inhibitor
3300 | SU 5402

IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively. Inhibits embryonic left-right determination and exhibits potent anticancer activity in vitro and in vivo.

Related Products: SU 6668 SU 5416 ZM 323881
P2X7 allosteric modulator
3385 | GW 791343

Exhibits species-specific activity; acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2) and a positive allosteric modulator of rat P2X7.

Related Products: A 438079 Ro 0437626 AZ 10606120

June 2009

Potent and selective PAR2 agonist
3369 | AC 55541

pEC50 = 6.7). Displays no activity at other PAR subtypes. Stimulates cell proliferation, PI hydrolysis and Ca2+ mobilization in vitro (pEC50 values are 6.7, 5.9 and 6.6 respectively) and exhibits pronociceptive activity in vivo.

Related Products: SLIGRL-NH2 SCH 79797 TFLLR-NH2
Selective, non-competitive AMPA antagonist
2932 | CP 465022

IC50 = 25 nM in rat cortical neurons. Displays potent anticonvulsant activity. Also significantly blocks the persistent component of Nav1.6 channel activity. Brain penetrant and orally active.

Related Products: GYKI 52466 (S)-AMPA GYKI 47261
Potent, broad spectrum MMP inhibitor
2961 | Batimastat

C50 values are 3, 4, 4, 6 and 20 nM for MMP -1, -2, -9, -7 and -3 respectively). Exhibits antiproliferative, anti-invasive and antimetastatic activity in human ovarian carcinoma xenografts in vivo.

Related Products: Marimastat ONO 4817 PD 166793
Potent and selective ATM kinase inhibitor
3544 | KU 55933

Ki = 2.2 nM, IC50 values are 13, 2500, 9300, 16600, >100000 and > 100000 nM at ATM, DNA-PK, mTOR, PI 3-K, PI 4-K and ATR respectively. Decreases viability of MCF-7, A549 and HCT116 cells and decreases p21CIP1 levels in vitro.

Related Products: CGK 733 Mirin NSC 109555
Potent ErbB receptor family inhibitor
3352 | JNJ 28871063

IC50 values are 21, 22 and 38 nM for ErbB4, EGFR and ErbB2 respectively). Displays potent growth inhibition of human cancer cell lines overexpressing ErbB2 in vitro (IC50.

Related Products: Iressa AG 490 PD 198306

May 2009

Potent, selective mGlu5 antagonist
2921 | MTEP hydrochloride

IC50 = 5 nM in Ca2+-flux assay; Ki= 16 nM. Displays anxiolytic activity in vivo and is orally active.

Related Products: MPEP CDPPB CHPG
Antiangiogenic. Heparanase inhibitor
2710 | OGT 2115

IC50 = 0.4 μM). Displays no major inhibition of human cytochrome P450 isoenzymes (IC50 > 30 μM). Exhibits antiangiogenic properties in vitro (IC50 = 1 μM).

Related Products: Heparin sodium salt
Voltage-independent, CFTR channel blocker
3430 | CFTRinh 172

Ki = 300 nM. Blocks intestinal fluid secretion induced by cholera toxin and Escherichia coli and suppresses cyst growth in animal models of polycystic kidney disease. Orally active.

Related Products: Chromanol 293B Lonidamine Glibenclamide
Potent and selective CK1ε and CK1δ inhibitor
3316 | PF 670462

IC50 values are 7.7 and 14 nM for CK1ε and CK1δ respectively. Displays > 30 fold selectivity over 42 other common kinases. Attenuates methamphetamine-stimulated locomotion in vivo.

Related Products: D 4476
Potent P2X7 receptor antagonist
3323 | AZ 10606120

KD values are 1.4 and 19 nM at human and rat P2X7 receptors respectively. Binds in a positive cooperative manner to sites distinct from, but coupled to, the ATP binding site and acts as a negative allosteric modulator.

Related Products: BzATP A 438079 KN-62

April 2009

Selective protein kinase D inhibitor
3327 | CID 755673

IC50 values are 0.182, 0.280, 0.227, >10, 15.3, 20.3, 40.5 and >50 μM at PKD1, PKD2, PKD3, PKC, CAK, PLK1, CAMKIIα and Akt respectively. Inhibits prostate cancer cell proliferation, migration and invasion in vitro.

Related Products: GF 109203X R 59-022 Phorbol 12-myristate 13-acetate
Selective mGlu1 antagonist
3060 | A 841720

Displays 34-fold selectivity over mGlu5m (IC50 values are 10 and 342 nM respectively). Exhibits analgesic effects; decreases mechanical allodynia in models of neuropathic pain. Also impairs cognitive function.

Related Products: CDPPB LY 456236 YM 298198
Potent and selective α7 nAChR agonist
3092 | PHA 543613

Displays selectivity over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. Positively influences sensory gating and memory in in vivo models of schizophrenia. Orally active and brain penetrant.

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Potent and selective γ-secretase inhibitor
2627 | L-685,458

IC50 = 17 nM. Displays > 50-fold selectivity over a range of aspartyl, serine and cysteine proteases. Exhibits equal potency for inhibition of Aβ40 and Aβ42 peptides (IC50 values are 48 and 67 nM respectively in human neuroblastoma cells).

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Potent and selective OX2 antagonist
3371 | TCS OX2 29

IC50 = 40 nM. Displays > 250 fold selectivity over OX1 and 50 other receptors, ion channels and transporters.

Related Products: [Ala11,D-Leu15]-Orexin B SB 334867 Orexin A (human, rat, mouse)

March 2009

Subtype-selective GABAA partial agonist
3250 | L-838,417

Selectively binds to α1, α2, α3 and α5 subunits (Ki values are 0.79, 0.67, 0.67 and 2.25 nM respectively) but displays no efficacy at α1 (α1-sparing). Exhibits non-sedative anxiolytic, antinociceptive and anti-inflammatory activity in vivo.

Related Products: Muscimol SR 95531 (-)-Bicuculline
Non-steroidal androgen receptor antagonist
3389 | Bicalutamide

IC50 = 190 nM. Displays peripheral selectivity and does not effect serum levels of LH and testosterone. Exhibits potent anticancer activity in vivo.

Related Products: Nilutamide Testosterone
Potent aromatase (CYP19) inhibitor
3388 | Anastrozole

IC50 = 15nM. Displays no discernible effect on adrenocorticoid hormone synthesis. Reduces plasma estrogen levels and exhibits antitumor activity in vivo. Orally active.

Related Products: YM 511 ICI 182,780 PPT
JAK2, FLT3 and TrkA inhibitor
3395 | Lestaurtinib

IC50 values are 0.9, 3 and > 25 nM for JAK2, FLT3 and TrkA respectively. Prevents STAT5 phosphorylation (IC50 = 20 - 30 nM). Exhibits antiproliferative activity in vitro and is effective against myeloproliferative disorders in vivo.

Related Products: Cucurbitacin I GW 441756 ZM 449829
Potent, selective p38α and p38β inhibitor
2999 | RWJ 67657

IC50 values are 1 and 11 μM for p38α and p38β respectively. Displays no activity at p38γ, p38δ and a range of other kinases. Exhibits cardioprotective and anti-inflammatory activity in vivo. Orally active.

Related Products: SB 203580 JX 401 SD 169

February 2009

Positive allosteric modulator at mGlu5
3235 | CDPPB

EC50 values are 10 and 20 nM for human and rat receptors respectively. Antipsychotic; reverses amphetamine-induced locomotor activity and amphetamine-induced deficits in prepulse inhibition in rats.

Related Products: VU 0155041 LY 354740 MMPIP
Selective GABAB positive allosteric modulator
3313 | rac BHFF

Increases the potency and efficacy of GABA ( > 15-fold and > 149% respectively). Exhibits anxiolytic activity in vivo and is orally active.

Related Products: CGP 7930 GS 39783 CGP 55845
Potent Chk1 inhibitor
3038 | TCS 2312

Ki = 0.38 nM, EC50 = 60 nM. Enhances the cell killing activity of Gemcitabine (Cat. No. 3259) in breast and prostate cancer cell lines and displays antiproliferative effects in vitro.

Related Products: SB 218078 PD 407824 Mirin
Highly selective CXCR4 antagonist
3299 | AMD 3100

IC50 values are 0.02 - 0.13 and > 25 μM for CXCR4 and all other chemokine receptors respectively. Switches inflammatory responses from Th2 to Th1 type and reduces airway hyperresponsiveness in a mouse model of asthma.

Related Products: BMS CCR2 22 SB 265610 ZK 756326
Selective Pim-1 kinase inhibitor
2979 | TCS PIM-1 1

IC50 values are 50, > 20000 and > 20000 nM for Pim-1, Pim-2 and MEK1/2 respectively.

Related Products: NSC 95397 NSC 663284

January 2009

Dual cdc7/cdk9 inhibitor
3140 | PHA 767491

IC50 values are 10 and 34 nM respectively. Prevents inititaion of DNA replication and inhibits cell proliferation in a variety of human cell lines (IC50 ~ 0.86 - 5.87 ÁM).

Related Products: 5-Iodo-A-85380 Ryuvidine SU 9516
Selective P2X1 antagonist
2188 | Ro 0437626

IC50 = 3 μM. Displays > 30-fold selectivity over P2X2, P2X3 and P22/3 receptors (IC50 > 100 μM).

Related Products: RO-3 Spinorphin A 438079
Microtubule depolymerization agent
3101 | XRP44X

Ras-Net (Elk-3) pathway inhibitor (IC50 = 10-20 nM). Indirectly inhibits Net phosphorylation upstream of Erk1/2 activation. Inhibits angiogenesis and acts as a microtubule depolymerizing agent in vitro.

Related Products: Combretastatin A4 Flutax 1 D-64131
Potent aromatase (CYP19) inhibitor
3278 | YM 511

IC50 values are 0.4 and 0.12 nM at rat ovary and human placenta cells respectively. Only weakly inhibits the synthesis of other steroid hormones. Reduces plasma estrogen levels into ranges induced by ovariectomy.

Related Products: Testosterone Nilutamide Metyrapone
Potent non-competitive NMDA receptor antagonist
3125 | Conantokin-R

IC50 = 93 nM. Suggested to have NR2 subunit selectivity. Exhibits broad anticonvulsant and antiparkinsonian activity in vivo at doses devoid of behavioral toxicity.

Related Products: Conantokin-T Co 101244 D-AP5

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